Zobrazeno 1 - 10
of 23
pro vyhledávání: '"Alec D. Lebsack"'
Autor:
Mark S. Tichenor, John J. M. Wiener, Navin L. Rao, Genesis M. Bacani, Jianmei Wei, Charlotte Pooley Deckhut, J. Kent Barbay, Kevin D. Kreutter, Leon Chang, Kathleen W. Clancy, Heather E. Murrey, Weixue Wang, Kay Ahn, Michael Huber, Elizabeth Rex, Kevin J. Coe, Jiejun Wu, Haopeng Rui, Kia Sepassi, Marcello Gaudiano, Mariette Bekkers, Ivo Cornelissen, Kathryn Packman, Mark Seierstad, Christos Xiouras, Scott D. Bembenek, Richard Alexander, Cynthia Milligan, Sriram Balasubramanian, Alec D. Lebsack, Jennifer D. Venable, Ulrike Philippar, James P. Edwards, Gavin Hirst
Publikováno v:
Journal of Medicinal Chemistry. 65:14326-14336
Bruton's tyrosine kinase (BTK) is a Tec family kinase that plays an essential role in B-cell receptor (BCR) signaling as well as Fcγ receptor signaling in leukocytes. Pharmacological inhibition of BTK has been shown to be effective in treating hemat
Autor:
Jennifer D. Venable, Weixue Wang, Jianmei Wei, Heather E. Murrey, Mark S. Tichenor, Kristi A. Leonard, Michael Huber, Alec D. Lebsack, Genesis M. Bacani, Scott D. Bembenek, Kay Ahn, J. Kent Barbay, Leon Chang, Kevin D. Kreutter, Navin Rao, Charlotte Pooley Deckhut, Jiejun Wu, Kevin J. Coe, Elizabeth B. Rex, John J. M. Wiener, James P. Edwards, Mark Seierstad
Publikováno v:
ACS Med Chem Lett
[Image: see text] Bruton’s tyrosine kinase (BTK) is a cytoplasmic tyrosine kinase that plays a critical role in the activation of B cells, macrophages, and osteoclasts. Given the key role of these cell types in the pathology of autoimmune disorders
Autor:
Alec D. Lebsack, Alan D. Wickenden, Sandra R. Chaplan, Qi Wang, Jason C. Rech, Love Christopher John, William A. Eckert, J. Guy Breitenbucher, Ludwig Paul Cooymans, Leenaerts Joseph Elisabeth, Anindya Bhattacharya, Bryan James Branstetter, Hong Ao
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 26:4781-4784
The synthesis, SAR and preclinical characterization of a series of 6-chloro- N -(2-(4,4-difluoropiperidin-1-yl)-2-(2-(trifluoromethyl)pyrimidin-5-yl)ethyl)quinoline-5-carboxamide based P2X7 antagonists is described herein. The lead compounds are pote
Autor:
Taraneh Mirzadegan, Navin Rao, Alec D. Lebsack, Kelly L. Damm-Ganamet, Nidhi Arora, John J. M. Wiener, James P. Edwards, Stéphane Bécart, Lori Westover, Marina I. Nelen, Heather M. McAllister
Publikováno v:
Journal of chemical information and modeling. 59(5)
At the onset of a drug discovery program, the goal is to identify novel compounds with appropriate chemical features that can be taken forward as lead series. Here, we describe three prospective case studies, Bruton Tyrosine Kinase (BTK), RAR-Related
Autor:
Curt A. Dvorak, Mandana Tootoonchi, Marcos E. Milla, Paul J. Krawczuk, Wendy Eccles, Xuejun Liu, Navin Rao, Jiejun Wu, John M. Keith, Steven P. Meduna, Jiao Song, Jonathan M. Blevitt, Jian Zhu, Alec D. Lebsack
Publikováno v:
SLAS Discovery. 21:127-135
Leukotrienes (LTs) and related species are proinflammatory lipid mediators derived from arachidonic acid (AA) that have pathological roles in autoimmune and inflammatory conditions, cardiovascular diseases, and cancer. 5-Lipoxygenase activating prote
Autor:
Stefan Steinbacher, Annie X. Liu, Paul F. Jackson, Marina I. Nelen, Marcos E. Milla, Krystal Herman, Aaron N. Patrick, Jonathan M. Blevitt, Paul J. Krawczuk, Kevin J. Lumb, Alec D. Lebsack, Taraneh Mirzadegan, Michael D. Hack
Publikováno v:
Journal of medicinal chemistry. 60(8)
A prevalent observation in high-throughput screening and drug discovery programs is the inhibition of protein function by small-molecule compound aggregation. Here, we present the X-ray structural description of aggregation-based inhibition of a prot
Autor:
Michael P. Maher, Sandra R. Chaplan, Jing Liu, Jason C. Rech, Brian Scott, William A. Eckert, Bryan James Branstetter, Hong Ao, Anne E. Fitzgerald, Yi Liu, Nyantsz Wu, Michele C. Rizzolio, Anindya Bhattacharya, Jamie M. Freedman, Alec D. Lebsack, Nadia Swanson, J. Guy Breitenbucher, Dong H. Li, Alan D. Wickenden, Kia Sepassi, Mena Kansagara
Publikováno v:
European Journal of Pharmacology. 663:40-50
As an integrator of multiple nociceptive and/or inflammatory stimuli, TRPV1 is an attractive therapeutic target for the treatment of various painful disorders. Several TRPV1 antagonists have been advanced into clinical trials and the initial observat
Autor:
Michelle Herrmann, Brett D. Allison, Alec D. Lebsack, Nadia Swanson, Hong Ao, Johnathan C. Buma, Brian Scott, J. Guy Breitenbucher, Jason C. Rech, Bryan James Branstetter, Alan D. Wickenden, Raymond Rynberg, Michael P. Maher, Sandra R. Chaplan, Anindya Bhattacharya, Lin Luo, Qi Wang, Michele C. Rizzolio, Natalie A. Hawryluk, Jamie M. Freedman, Jeffrey E. Merit
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:7142-7146
Based upon a previously reported lead compound 1, a series of 1,2-diamino-ethane-substituted-6,7,8,9-tetrahydro-5H-pyrimido[4,5-d]azepines were synthesized and evaluated for improved physiochemical and pharmacokinetic properties while maintaining TRP
Discovery and synthesis of 6,7,8,9-tetrahydro-5H-pyrimido-[4,5-d]azepines as novel TRPV1 antagonists
Autor:
Qi Wang, J. Guy Breitenbucher, Hong Ao, Michael D. Hack, Bryan James Branstetter, Alan D. Wickenden, Jamie M. Freedman, Alec D. Lebsack, Nadia Swanson, Michael P. Maher, Sandra R. Chaplan, Natalie A. Hawryluk, Jeffrey E. Merit, Brian Scott, Anindya Bhattacharya
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:7137-7141
Utilization of a tetrahydro-pyrimdoazepine core as a bioisosteric replacement for a piperazine-urea resulted in the discovery a novel series of potent antagonists of TRPV1. The tetrahydro-pyrimdoazepines have been identified as having good in vitro a
Autor:
Salony Maniar, Russell B. Lingham, Benito Munoz, Michael F. Gardner, Kenneth Alves, Alec D. Lebsack, Shankar Venkatraman, Joyce K. James, Qian Si, Bowei Wang, Richard A. Mumford, Nicholas Stock, Kelly M. Treonze, Jasmine Zunic
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:5803-5806
A series of prolyl-N-isonicotinoyl-(L)-4-aminophenylalanine derivatives substituted at the proline 4-position with cyclic amines was evaluated as VLA-4 antagonists. The ring size and presence or absence of fluorine affected potency and receptor occup